Engineering Research Centre of Pharmaceutical Process Chemistry, Ministry of Education, School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, China.
Chem Commun (Camb). 2012 Sep 21;48(73):9180-2. doi: 10.1039/c2cc34321e. Epub 2012 Aug 6.
A diamine-catalyzed asymmetric tandem reaction between α,β-unsaturated ketones and rhodanine derivatives has been developed to synthesize various spirocyclic compounds with high stereoselectivities (up to 99% ee and >20:1 dr). The products obtained contain two pharmaceutically relevant features: the biologically active rhodanine moiety embedded in a spirocyclic unit.
一种二胺催化的α,β-不饱和酮和罗定酸衍生物的不对称串联反应已被开发出来,用于合成具有高对映选择性(高达 99%ee 和 >20:1dr)的各种螺环化合物。得到的产物包含两个具有药物相关特征的部分:生物活性的罗定酸部分嵌入在螺环单元中。